PubMed Health⌕ Search

Biomedical subjects

A Nagaraju

Publications and source records attributed to A Nagaraju.

6 recordsLinked to original sources
PubMed2002

Computer-aided design of selective COX-2 inhibitors: comparative molecular field analysis, comparative molecular similarity indices analysis, and docking studies of some 1,2-diarylimidazole derivatives.

Comparative molecular field analysis and comparative molecular similarity indices analysis were performed on 114 analogues of 1,2-diarylimidazole to optimize their cyclooxygenase-2 (COX-2) selective antiinflammatory activities. These studies produced models with high correlation coefficients and good predictive abilities. Docking studies were also carried out wherein these analogues were docked into the active sites of both COX-1 and COX-2 to analyze the receptor ligand interactions that confer selectivity for COX-2. The most active molecule in the series (53) adopts an orientation similar to that of SC-558 (4-[5-(4-bromophenyl)-3-trifluoromethyl-1H-1-pyrozolyl]-1-benzenesulfonamide) inside the COX-2 active site while the least active molecule (101) optimizes in a different orientation. In the active site, there are some strong hydrogen-bonding interactions observed between residues His90, Arg513, and Phe518 and the ligands. Additionally, a correlation of the quantitative structure-activity relationship data and the docking results is found to validate each other and suggests the importance of the binding step in overall drug action.

Binding Sites↗
PubMed1982

Flutroline in the treatment of the schizophrenic patient.

As an introduction into a clinical study of one of a new group of compounds having neuroleptic potential, the background and characteristics of the gamma carbolines, particularly flutroline, are cited in the general context of a review of the use of antipsychotic drugs in psychiatry. In the four-week double-blind trial involving dosages of 1, 5, 10, 20 and 100 mg, 48 hospitalized schizophrenic patients were given the tryptoline derivative flutroline on a once-a-day basis. Outcome criteria obtained weekly, including the incidence of side effects, standardized psychiatric ratings, and clinical global impressions of psychopathology, indicated that flutroline was a safe and effective antipsychotic drug. Data suggested that dosages of 20 mg and above offered the best potential for optimal clinical effectiveness.

Adolescent↗
PubMed1981

Viloxazine and the depressed schizophrenic--methodological issues.

A pilot study of a small group of schizophrenic patients manifesting symptoms of a depressive nature was treated in a double-blind study in which viloxazine or a placebo was administered in combination with either chlorpromazine or haloperidol. There appeared to be no difference between the viloxazine-treated group and the placebo-treated group, although the study raised some question as to the adequacies of the dosage utilized since there was an absence of any apparent side effects. In view of these issues concerning the clinical merit of the combination, this obviously requires further investigation.

Adult↗
PubMed1980

The dopamine radioreceptor assay--a clinical application.

The counterbalanced design in a bioequivalent study of haloperidol indicated an absence of any clinical difference between a new 20-mg dosage form and two 10-mg tablets of haloperidol (Haldol). This impression was supported by the absence of any significant behavioral changes during the four weeks when either form of the once-a-day fixed dose of 20 mg haloperidol was administered. This impression was substantiated by experiences with the dopamine receptor blocking assay, since results with this procedure also indicated the lack of any significant difference in the plasma neuroleptic equivalence of either dosage form. On the basis of present findings the assay would appear to offer promise for clinical application in the adjusting of the dosage of neuroleptic drugs, as well as in the monitoring of drug usage.

Adult↗
PubMedDate not supplied

The prolactin response to flutroline hydrochloride in schizophrenic patients.

Flutroline hydrochloride, a gamma carboline manifesting neuroleptic activity, was administered in a double-blind fashion in single daily dosages of 1, 5, 10, 20, and 100 mg to 48 hospitalized schizophrenic patients over a period of four weeks. During this period, weekly evaluations were made of response employing standardized psychiatric ratings. Plasma prolactin (PRL) levels were obtained at the termination of previous neuroleptic medication and at two-week intervals during treatment with the investigational compound. Examination of the initial PRL levels indicated that they could be grouped into those above, within, and below the normal range. Comparisons of these initial levels with those following the administration of flutroline suggested an improved methodology for determining optimal neuroleptic dosage.

Adolescent↗